| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 100mg | |||
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| Targets |
DC_517 targets DNA methyltransferase 1 (DNMT1). DNMT1 is an epigenetic enzyme responsible for maintaining DNA methylation patterns during cell division, which regulates gene expression. Inhibition of DNMT1 leads to the reactivation of tumor suppressor genes and other epigenetically silenced genes, which can suppress tumor growth.
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| ln Vitro |
DC_517 is a DNMT1 inhibitor with IC50 and Kd values of 1.7 μM and 0.91 μM, respectively. DC_517 (1.25, 2.5, 5 and 10 μM) substantially suppressed the growth of HCT116 (human colon cancer) and Capan-1 (human pancreatic adenocarcinoma cells) after 24, 48, and 72 hours of treatment. DC_517 (0, 0.75, 1.5, and 3 μM) causes apoptosis in HCT116 cells in a dose-dependent manner [1].
In vitro, DC_517 is a potent DNMT1 inhibitor with an IC50 of 1.7 μM and a binding affinity (Kd) of 0.91 μM. It substantially suppresses the growth of HCT116 (human colon cancer) and Capan-1 (human pancreatic adenocarcinoma) cells at concentrations of 1.25, 2.5, 5, and 10 μM after 24, 48, and 72 hours of treatment. It also induces apoptosis in HCT116 cells in a dose-dependent manner at concentrations of 0.75, 1.5, and 3 μM. |
| ln Vivo |
No specific in vivo animal data is publicly available for DC_517. While one source mentions intravenous (i.v.) and oral (p.o.) administration in a pharmacokinetic context, detailed in vivo efficacy or animal model studies have not been reported in the available literature. The compound is primarily characterized in vitro.
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| Enzyme Assay |
In cell-free enzymatic assays, the activity of DC_517 is evaluated by measuring its inhibition of DNMT1 catalytic activity. The assay typically involves incubating purified recombinant DNMT1 enzyme with its substrate (e.g., a DNA oligomer containing a hemimethylated CpG site) and the methyl donor S-adenosylmethionine (SAM) in the presence of varying concentrations of DC_517. The extent of methylation is then quantified, and the IC50 value is calculated from the inhibition curve.
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| Cell Assay |
Cell-based assays for DC_517 typically involve culturing cancer cell lines such as HCT116 (human colon cancer) or Capan-1 (human pancreatic adenocarcinoma). Cells are seeded in multi-well plates and treated with various concentrations of DC_517 (e.g., 1.25, 2.5, 5, and 10 μM) for 24, 48, or 72 hours. Cell proliferation and viability are then assessed using standard assays such as MTT or CellTiter-Glo. Apoptosis induction can be measured by flow cytometry after Annexin V/PI staining.
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| Animal Protocol |
No specific in vivo animal protocols are publicly available for DC_517. The compound's effects have been primarily characterized in vitro. No standard animal models have been reported in the available literature.
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| ADME/Pharmacokinetics |
No detailed pharmacokinetic data is publicly available for DC_517. One source provides preliminary data showing that after i.v. (2 mg/kg) and p.o. (10 mg/kg) administration, the compound exhibited a half-life of 6.7 hours in both routes, with an oral bioavailability of 38.7%. Further comprehensive PK parameters are not reported.
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| Toxicity/Toxicokinetics |
No specific toxicity data is publicly available for DC_517. As a research compound, its safety profile in vivo has not been established. In cell-based assays, it shows antiproliferative and pro-apoptotic effects at micromolar concentrations. The compound is for research use only and is not for human therapeutic use.
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| References | |
| Additional Infomation |
DC_517 belongs to the carbazole class of compounds, with the chemical name 1,3-di(9H-carbazole-9-yl)prop-2-ol, in which the hydroxyl group is replaced by 2-hydroxy-3-[(prop-2-yl)amino]propoxy. It is a DNA methyltransferase 1 inhibitor (IC50 = 1.7 μM). It has multiple functions, including as an EC 2.1.1.37 [DNA (cytosine-5-)-methyltransferase] inhibitor, an apoptosis inducer, and an antitumor drug. It belongs to the carbazole class, ether class, secondary amine class, secondary alcohol class, and tertiary amine class of compounds.
DC_517 is a selective DNMT1 inhibitor with the IUPAC name 1-[1,3-di(carbazol-9-yl)propan-2-yloxy]-3-(propan-2-ylamino)propan-2-ol. Its molecular formula is C33H35N3O2 and its molecular weight is 505.65. It is a member of the carbazoles chemical class. It is used as a research tool to study DNA methylation, gene regulation, and epigenetic therapeutic strategies. |
| Molecular Formula |
C33H35N3O2
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|---|---|
| Molecular Weight |
505.66
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| Exact Mass |
505.272
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| Elemental Analysis |
C, 78.38; H, 6.98; N, 8.31; O, 6.33
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| CAS # |
500017-70-9
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| PubChem CID |
3713657
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
727.9±60.0 °C at 760 mmHg
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| Flash Point |
394.0±32.9 °C
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| Vapour Pressure |
0.0±2.5 mmHg at 25°C
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| Index of Refraction |
1.644
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| LogP |
8.26
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
38
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| Complexity |
654
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC(C)NCC(COC(CN1C2=CC=CC=C2C3=CC=CC=C31)CN4C5=CC=CC=C5C6=CC=CC=C64)O
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| InChi Key |
BLTONWSCODZCNA-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C33H35N3O2/c1-23(2)34-19-24(37)22-38-25(20-35-30-15-7-3-11-26(30)27-12-4-8-16-31(27)35)21-36-32-17-9-5-13-28(32)29-14-6-10-18-33(29)36/h3-18,23-25,34,37H,19-22H2,1-2H3
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| Chemical Name |
1-[1,3-di(carbazol-9-yl)propan-2-yloxy]-3-(propan-2-ylamino)propan-2-ol
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| Synonyms |
DC517; DC 517; DC_517
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 50 mg/mL (~98.88 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 3.25 mg/mL (6.43 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 32.5 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 3.25 mg/mL (6.43 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 32.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 3.25 mg/mL (6.43 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9776 mL | 9.8881 mL | 19.7761 mL | |
| 5 mM | 0.3955 mL | 1.9776 mL | 3.9552 mL | |
| 10 mM | 0.1978 mL | 0.9888 mL | 1.9776 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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